One-step labelling of a novel small-molecule peptide with astatine-211: preliminary evaluation in vitro and in vivo
One-step labelling of a novel small-molecule peptide with astatine-211: preliminary evaluation in vitro and in vivo
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DOI：
10.1007/s10967-018-5780-x
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发表时间：
2018-03
影响因子：
1.6
通讯作者：
Weihao Liu;Huan Ma;Yurong Tang;Qingsong Chen;Shuqun Peng;Jijun Yang;J. Liao;Yuanyou Yang;Qian-wei Li;Ning Liu
中科院分区：
文献类型：
--
作者：
Weihao Liu;Huan Ma;Yurong Tang;Qingsong Chen;Shuqun Peng;Jijun Yang;J. Liao;Yuanyou Yang;Qian-wei Li;Ning Liu
本文采用一步法（先偶联双功能中间体SPC再标记）对新型小分子融合肽VP 2进行了211 At标记，放化产率约为45%。在室温下24小时后，放射化学纯度仍> 95%。体外特异性研究表明，211 At-SPC-VP 2对多种肿瘤细胞具有较高的亲和力。此外，211 At-SPC-VP 2在KM小鼠体内的生物分布表明，211 At-SPC-VP 2在体内具有足够的稳定性。本研究表明，采用该方法制备的211 At-SPC-VP 2有望成为一种新型的肿瘤放射治疗靶向药物。
In this paper, VP2, a novel small molecule fusion peptide, was labelled with211At through a one-step method (coupled with bifunctional intermediate SPC first and then labelled) with a radiochemical yield of about 45%. The radiochemical purity was still > 95% after 24 h at room temperature. Specificity studies in vitro indicated that211At-SPC-VP2 has a high affinity for several tumour cells. Additionally, biodistribution in KM mice showed that211At-SPC-VP2 has sufficient stability in vivo. This research suggested that211At–SPC-VP2 produced by the convenient method has the potential to be a novel targeted drug for cancer radiotherapy.